Major General James G. Blunt

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Tenilapine is an atypical antipsychotic which has never been marketed in the US.

Pharmacodynamics

Tenilapine has a relatively high affinity for the 5-HT2A receptor, and relatively low (micromolar) affinities for dopamine receptors.

Binding affinities
Receptor Ki (nM)
D2 1584[1]
D4 721±300[1]
5-HT2A 40[1]

The ratio of D2 to D4 bonding is similar to that of clozapine.[1] Like many other atypical antipsychotics, it is a potent 5-HT2C antagonist.[2]

References

  1. ^ a b c d Roth BL, Tandra S, Burgess LH, Sibley DR, Meltzer HY (August 1995). "D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs". Psychopharmacology (Berl). 120 (3): 365–8. doi:10.1007/BF02311185. PMID 8524985. S2CID 13549491.
  2. ^ Di Giovanni G, Esposito E, Di Matteo V (2011). "The 5-HT2C Receptor Subtype Controls Central Dopaminergic Systems: Evidence from Electrophysiological and Neurochemical Studies". 5-HT2C Receptors in the Pathophysiology of CNS Disease. The Receptors. Vol. 22. Totowa, NJ: Humana Press. pp. 215–247. doi:10.1007/978-1-60761-941-3_11. ISBN 978-1-60761-940-6.